• Archives of Pharmacal Research
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• 제27권6호
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• pp.600-603
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• 2004

(＋）-Dehydrovomifoliol (1）. 3-hydroxy-5$\alpha$,6$\alpha$-epoxy-$\beta$-ionone (2）, vitexin 7 -O-$\beta$-D-glucopyrano-side (3）, and vitexin 2'-O-$\beta$-D-glucopyranoside (4） were isolated as new constituents from the aerial parts of Beta vulgaris var. cicla. Compounds 3 and 4 demonstrated hepatoprotective activity with values of 65.8 and 56.1％, respectively, in primary cultured rat hepatocytes with $CCl_4$-induced cell toxicity, compared to controls. This was comparable to that of silibinin (69.8％） which was used as a positive control.trol.

• Archives of Pharmacal Research
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• 제26권10호
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• pp.773-777
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• 2003

In this study, some new nitroimidazole derivatives were obtained from 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethylamine dihydrochloride (4) and 1-(2-bromoethyl)-2-methyl-5-nitroimidazole (5), which were prepared using metronidazole. Compound 4 was reacted with arylisothiocyanates (6) to obtain 1-[2-(2-methyl-5-nitroimidazol-1-yl)ethyl]-3-arylthioureas (7) and the latter with $\alpha$-bromoacetophenones (8) to give -3-[2-(2-methyl-5-nitroimidazol-1-yl)ethyl]-2-arylimino-4-aryl-4-thiazolines (9). Also 1-[2-(2-methyl-5-nitroimidazol-1-yl)ethyl]-2-phenyl-4-arylideneimidazolin-5-ones (11) were prepared by reaction of 4 with 2-phenyl-4-arylidene-5-oxazolones (10). The reaction of the other starting material 5 with 5-arylidenethiazolidin-2,4-dione (12) gave 3-[2-(2-methyl-5-nitroimidazol-1-yl)ethyl]-5-arylidenethiazolidin-2,4-dione (13) derivatives. Structural elucidation of the compounds was performed by IR, $^1H-NMR$ and MASS spectroscopic data and elemental analysis results. Antimicrobial activities of the compounds were examined and moderate activity was obtained.

• Archives of Pharmacal Research
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• 제29권10호
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• pp.821-825
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• 2006

Two isoflavone C-glucosides, puerarin (1) and PG-3 (2), a but-2-enolide, $({\pm})-puerol$ B (3), two isoflavone O-glucosides, daidzin (4) and genistin (5), and three pterocarpans, (-)-medicarpin (6), (-)-glycinol (7) and (-)-tuberosin (8), were isolated from a MeOH extract of the roots of Pueraria Iobata, using an in vitro bioassay based on the inhibition of the formation of advanced glycation end products (AGEs) to monitor chromatographic fractionation. The structures of 1-8 were determined by spectroscopic data interpretation, particularly by 1D- and 2D-NMR studies, and by comparison of these data with values in the literature. All of the isolates (1-8) were evaluated for their inhibitory activity on AGEs formation in vitro. Of these, puerarin (1), PG-3 (2), and $({\pm})-puerol$ B (3) exhibited more potent inhibitory activity than the positive control aminoguanidine.

• Archives of Pharmacal Research
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• 제22권2호
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• pp.151-156
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• 1999

Despite the impressive antitumor activity of cisplatin, two major limitations of the drug, that is severe side effects and drug-resistance of cancer cells, make its use difficult of r cancer therapy. These limitations have resulted in a greate deal of effort having been expended into structural modifications of cisplatin. In this study, we tested two novel cisplatin analogues, (CPA)2 Pt[DOLYM] (COMP-I) and (DACH)Pt[DOLYM] (CoMP-II), for the mode of cytotoxic action against human tumor cells comparing with cisplatin and carboplatin in vitro. These two novel analogues had considerable cytotoxic activities against five kinds of human solid tumor cells, and especially COMP-II was more effective on HCT15 colon cancer cells than other compounds. In addition, COMP-II had cytostatic activity at low concentrations (10~0.3${\mu}g/ml$), but other compounds revealed little effect on tumor growth at the low concentration.

• Archives of Pharmacal Research
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• 제21권1호
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• pp.67-69
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• 1998

Three TNF-$\alpha$inhibitory lignans were isolated from the flower buds of Magnolia fargesii through bioassay-guided isolation. They were identified as eudesmin, magnolin and lirioresinol-B dimethylether on the basis of their spectroscopic data. All three lignans showed inhibitory effects on TNF-$\alpha$ production in LPS-stimulated murine macrophage cell line, RAW264.7 and eudesmin showed the strongest activity ($IC_{50}=51{\mu}M)$.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.253.1-253.1
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• 2003

Twenty-seven N,N',N"-trisubstituted thiourea derivatives were prepared. Among them, 1- [3-(4'-hydroxy-3'-methoxy-phenyl)-propyl] -1,3-diphenethyl-thiourea (81, IC$\sub$50/= 0,32 $\mu\textrm{m}$), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC$\sub$50/= 0,65 $\mu\textrm{m}$) against the vanilloid receptor in a Ca$\^$2+/ -influx assay.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1988년도 학술대회지
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• pp.147-150
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• 1988

망내계에서 강한 탄소제거 활성을 나타내는 다당류를 Panax식물속에서 조사하였다. 건조한 P. notoginseng 에서 sanchinan-A라는 활성을 지닌 다당류를 분리하였다. Sanchinan-A의 분자량은 약 1,500,000 D 정도로 추정되며 6번 산소위치에 가지가 있는 $\beta$-D(1-3)-galactan 구조를 가지고 있다. 3개의 glactosyl units에 2개 정도의 빈도로 6번산소위치에 주로 $\alpha$-L-arabionfuranosyl이 있으며 일부는 $\beta$-galactopyranosyl-(1-6)-$\beta$-D-galactopyranosyl-(1-3)-$\beta$-D-galactopyranosyl 가지가 있다. 건조한 P. japonicus의 근경에서도 활성을 지닌 몇가지 다당류가 분리되어 그 구조가 규명되었다. 건조한 P. ginseng의 뿌리에서는 강한 활성을 지닌 몇가지 다당류가 분리되었다. 이들 화합물의 구조는 현재 구명중이다. 홍삼의 물 추출물에서는 활성을 보이지 않았으나 투석한 분획에서는 현저히 망내계기능을 강화시켰다. 그러나 이러한 활성도는 분리과정에서 소실되었다. 이러한 사실로 보아 인삼중에서는 활성물질을 안정화 시키는 어떤 물질이 그 분획중에 존재하기 때문인 것으로 사료된다.

• Journal of Photoscience
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• 제9권2호
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• pp.311-313
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• 2002

X-ray structures of pharaonis phoborhodopsin (ppR) show the different direction of the side chain of Arg72 from that of the corresponding residue (Arg82) of bacteriorhodopsin, BR. For BR, this residue is considered to play an important role in the proton pumping. In order to investigate the role of Arg72 in ppR, we constructed Arg72 mutants of R72A, R72K and R72Q, and measured the photocycle and proton pumping activities. The pH-titration curves on the absorption maximum of the mutants were shifted to alkaline in comparison of that of the wild-type. This may imply the increase of pKa of D75, suggesting the presence of the (probably electric) interaction between D75 and Arg72. Rate constants of the M-decay were 3-7 times faster than that of the wild-type, and the time for the completion of the photocycling was also reduced. Using Sn0$_2$ electrode, the rate of transmembrane proton transport was measured upon illumination. The photo-induced proton pumping activities were estimated after the corrections that are the percentages of the associated form of D75 (which has no pumping activity) and the photocycling rates. R72A and R72Q showed the reduced activity while R72K did not reduce the activity.

• 한국작물학회지
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• 제51권spc1호
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• pp.1-6
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• 2006

Tocotrienol의 건강식품 및 의료용 가공품으로의 고부가가치화 가능성을 평가하기 위하여 미강에서 추출한 tocotrienol의 항암 효과 및 독성평가를 실시하였다. HepG2 간암 세포를 대상으로 한 항암효과 분석 결과 tocotrienol이 간암세포의 증식을 억제함을 입증할 수 있었다. 또한 랫드를 이용한 경구독성 검사를 수행한 결과 tocotrienol 최종 생산물은 경구투여 한계량인 $2,000mg\;kg^{-1}$ 수준에서도 사망률, 일반 증상, 체중 변화 등에 이상을 보이지 않았으며, 부검 후 흉강 및 복강의 모든 장기에 대한 육안적 부검 소견 등에서도 아무런 독성학적 변화가 유발되지 않음을 알 수 있었다.

• 생약학회지
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• 제47권4호
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• pp.343-351
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• 2016

The purpose of this study was to evaluate the whitening effect of aerial part of Pueraria lobata and mechanisms. Aerial part of Pueraria lobata, dose-dependently reduced the melanin content. Aerial part of Pueraria lobata, significantly decreased cellular tyrosinase activity, while there was not any effect on tyrosinase in cell-free conditions. To elucidate the mechanisms behind the aerial part of Pueraria lobata, treated melanogenesis regulation, the expressions of melanogensis related genes, proteins, and the activity of ${\alpha}-glucosidase$ were determined. Aerial part of Pueraria lobata, significantly inhibited gene and protein levels of MITF, tyrosinase and TRP-1. It suppressed the ${\alpha}-glucosidase$, leading to inhibition on the maturation of tyrosinase. Also aerial part of Pueraria lobata, was observed to have the high antioxidant activity. These results suggested that whitening effect of aerial part of Pueraria lobata, should be due to the down-regulation of MITF, tyrosinase and TRP-1 expression and the intercepting maturation of tyrosinase through suppressing ${\alpha}-glucosidase$. Another should be the high anti-oxidant activity. The findings show the possibility that aerial part of Pueraria lobata, can be used as a potential skin-whitening agent.